Toloxatone

207.23

207.23

249-522-2

N - Nervous system

2934999090

49.8

1.2

1.245g/cm3

76 °C

333

170.9ºC

1.57

DMSO: >10mg/mL

2-8°C

8.9E-06mmHg at 25°C

LD50 orally in mice (mg/kg): 1850 (Fauran); also reported as 1500 (Raynaud)

III

6.1(b)

3249

3

22

RQ2867500

Xn

P264, P270, P301+P312, P330, P501

H302

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory.

In rare cases, toloxatone toxicity may cause fulminant hepatitis. More common adverse effects include dysuria, nausea, constipation, vertigo, and insomnia. Administration of toloxatone can lead to an increased risk of serotonin syndrome with selective serotonin reuptake inhibitors (SSRI), and tricyclic antidepressants. Increased blood pressure can occur with sympathomimetic medication coadministration. One study showed that when combined with meals, elevated doses of toloxatone may contribute to elevated blood pressure in healthy subjects. This pharmacodynamic interaction could be explained by enhanced tyramine bioavailability in the presence of toloxatone. This tyramine in meals and toloxatone is unlikely to occur in patients after long-term administration of the drug at therapeutic dosages.

For the treatment of major depressive disorder.

This drug has been shown to help manage the symptoms of depression by maintaining neuro-synaptic levels of serotonin and catecholamines while regulating their metabolism, which leads to relief of depressive symptoms.

Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems. (See all compounds classified as Antidepressive Agents.)|A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414) (See all compounds classified as Monoamine Oxidase Inhibitors.)

Mainly hepatic 1% of drug is excreted unchanged in the urine|High hepatic excretion rate

1-3 h

This medication is a reversible inhibitor of monoamine oxidase type-A (also known as RIMA). MAO-A can be found in norepinephrinergic and serotonergic neurons and regulates the metabolism of serotonin and catecholamines, allowing for increased circulation in the synaptic cleft. Traditional monoamine oxidase inhibitors irreversibly inhibit monoamine oxidase and therefore, side effects, drug interactions, and food interactions persist as long as 2-3 weeks after discontinuing toloxatone. The elevation of serotonin and norepinephrine levels occurs rapidly after medication administration. However, the therapeutic relief of depressive symptoms requires weeks of daily treatment to observe results. Selective and reversible MAO-A inhibitors are more effective in treating major depression without several of the drug and food interactions associated with traditional monoamine oxidase inhibitors.

(3-methyl)-3-phenyl-5-hydroxymethyl-2-oxazolidinone